Abstract: The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula ##STR1## in which R.sup.4 is .beta.-hydroxyl andR.sup.3 is .alpha.-ethyl; orR.sup.4 is hydrogen andR.sup.3 is .beta.-ethyl;R" is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >N.sub.a -CH.sub.2 -O-- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety;R.sup.1 is methoxy andR.sup.2 is acetyl,provided that if R.sup.3 is .alpha.-ethyl and R.sup.4 .beta.-hydroxyl, R.sup.4 is other than ethyl.

Abstract: The invention relates to a new method for controlling the level and distribution of alkaloids produced by Claviceps purpurea variant strains capable of producing primarily ergocornine, .alpha.-ergocryptine and .beta.-ergocryptine under saprophytic conditions. According to the invention a compound of the biosynthesis path of isoleucine or a compound which promotes the formation of isoleucine by biochemical control is added to the fermentation broth. In other respects fermentation is performed under conditions known per se.By the method of the invention the ratio of .alpha.- and .beta.-ergocryptine formed in the fermentation broth can be adjusted to the optimum value.

Abstract: A process for the preparation of diindole-alkaloids, especially new compounds corresponding to vinblastine or leurosine, in which the N-methyl group is replaced by an N--CH.sub.2 --O--R group wherein R is lower alkyl, having antitumor properties. The starting materials are subjected to oxidation by chromic acid or an alkali metal dichromate at temperatures from -90.degree. C. to -30.degree. C. and preferably below -45.degree. C. where the new compounds are to be produced, a lower alkanol being present in this case.

Abstract: A process for the preparation of diindolealkaloids, especially new compounds corresponding to vinblastine or leurosine, in which the N-methyl group is replaced by an N--CH.sub.2 --OC.sub.2 H.sub.5 group having antitumor properties. The starting compounds are subjected to oxidation by chromic acid or an alkali metal dichromate at temperatures from -90.degree. C. to -30.degree. C. but preferably below about -45.degree. C. when the new compounds are to be produced, ethanol being present in this case.

Abstract: Compounds of the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 each is saturated or unsaturated, straight-chained or branched alkyl phenyl, alkylphenyl or saturated or unsaturated cycloalkyl;but when R.sub.1 is methyl, R.sub.2 is a group other than methyl, are prepared by reacting a compound of the formula (II), ##STR2## wherein X is halogen, with a secondary amine of the formula (III),R.sub.1 --NH--R.sub.2 (III)The new compounds of the formula (I), as well as their pharmaceutically acceptable acid addition salts are active primarily in the induction of liver microsomal enzyme, but also possess antipyretic activity.

Abstract: New compounds of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 each is a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom forms a substituted or unsubstituted heterocyclic group with or without a further oxygen or nitrogen heteroatom, andR.sub.3 is hydrogen or an acyl group derived from a C.sub.1-18 carboxylic acid. The compounds are prepared by reducing the corresponding nitro compounds of the formula (II) ##STR2## and optionally acylating the obtained product. The compounds of the formula (I) and their acid addition salts and quaternary ammonium salts are active primarily in the induction of liver microsomal enzymes, but they also possess valuable antipyretic activity and a yohimbine lethality increasing effect characteristic of antidepressants.

Abstract: The invention relates to new 3-amino-17a-aza-D-homo-5.alpha.-androstane derivatives of the general formula I ##STR1## wherein R.sub.1 represents a methylene or an >N--CH.sub.3 group, and n stands for 1 or 2, and the acid addition salts and the quaternary salts of the general formula ##STR2## thereof, wherein R.sub.2 stands for an alkyl or alkenyl group having from 1 to 4 carbon atoms, and A represents a halogen atom, provided that if R.sub.1 stands for an >N--CH.sub.3 group, R.sub.2 is attached to the nitrogen of that >N--CH.sub.3 group. The new compound possess a non-polarizing neuromuscular blocking activity and have a short activity period.

Abstract: The invention relates to new .alpha.

Abstract: The invention is directed to a new substituted derivative of .alpha.-ethylnyl-benzophenone, namely, the 3-iodo-.alpha.-ethynyl-benzhydrol which has high antifungal activity.

Abstract: The new compound 3,4,5-trimethoxy-.alpha.-ethynyl benzhydrol which has been found to be an effective fungicide.

Abstract: .alpha.-ethynyl-benzhydrols, namely 2,5-dimethyl-.alpha.-ethynyl and 4-n-butyl-.alpha.-ethynyl benzhydrol, are made by reacting the starting benzophenone with acetylene in a solvent delivering no protons, in the presence of an alkali metal tertiary alcoholate, preferably potassium-ter.-butylate or potassium-tert.-amylate.

Abstract: New compounds of the general formula (I), ##STR1## wherein R.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom may form an optionally substituted heterocyclic group optionally containing a further oxygen or nitrogen hetero atom,But if R.sub.1 stands for methyl, R.sub.2 may only stand for a group other than methyl, are prepared by reacting a compound of the general formula ##STR2## wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2 (iii)wherein R.sub.1 and R.sub.2 each have the same meanings as defined above.The new compounds of the general formula (I), as well as their pharmaceutical acceptable acid addition salts or quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess antipyretic activity.

Abstract: A compound of the formula: ##STR1## wherein Z is ethyl or vinyl,R.sub.1 and R.sub.2 are hydrogen, lower alkyl, lower alkenyl or trihalomethyl,R.sub.3 and R.sub.4 are hydrogen, lower alkyl, lower alkenyl, trihalomethyl, cyclopentyl, benzyl or phenyl, andR.sub.5 is lower alkyl, lower alkenyl, trihalomethyl, cyclopentyl, benzyl, or phenyl with the proviso that where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each is hydrogen, R.sub.5 is not methyl attached to the 4-position of the benzene ring, or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof is disclosed as effective in the regulation of the liver microsomal enzyme system.

Abstract: New compounds of the general formula (I) ##SPC1##whereinR.sub.1 and R.sub.2 each is a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom may form substituted or unsubstituted heterocyclic group with or without a further oxygen or nitrogen heteroatom, andR.sub.3 is hydrogen or an acyl group derived from a C.sub.1.sub.-18 carboxylic acid.The compounds are prepared by reducing the corresponding nitro compounds of the general formula (II) ##SPC2##and optionally acylating the obtained product.The compounds of the general formula (I) and their acid addition salts and quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess valuable antipyretic activity and a yohimbine lethality increasing effect characteristic of antidepressants.

Abstract: New compounds of the general formula (I), ##SPC1##whereinR.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom may form an optionally substituted heterocyclic group optionally containing a further oxygen or nitrogen hetero atom,But if R.sub.1 stands for methyl, R.sub.2 may only stand for a group other than methyl,Are prepared by reacting a compound of the general formula (II), ##SPC2##wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2 (iii)wherein R.sub.1 and R.sub.2 each have the same meanings as defined above.The new compounds of the general formula (I), as well as their pharmaceutical acceptable acid addition salts or quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess antipyretic activity.

Abstract: The invention is a new process for the preparation of .alpha.-ethynyl-benzohydrols and of ring-substituted derivatives thereof by reacting the starting benzophenone or a ring-substituted derivative thereof with acetylene in a solvent delivering no protons, in the presence of an alkali metal tertiary alcoholate, preferably potassium-tert.-butylate or potassium-tert.-amylate. Also new substituted derivatives of .alpha.-ethynyl-benzhydrol are prepared by the invention.

Abstract: New compounds of the formula (I), ##SPC1##whereinR.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straightchained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom form a substituted or unsubstituted heterocyclic group which can contain a further oxygen or nitrogen hetero atom,But when R.sub.1 is methyl, R.sub.2 is a group other than methyl, are prepared by reacting a compound of the formula (II), ##SPC2##wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2. (iii)the new compounds of the general formula (I), as well as their pharmaceutical acceptable acid addition salts or quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess antipyretic activity.